EP2968275A4 - Modulateurs des lxr - Google Patents

Modulateurs des lxr

Info

Publication number
EP2968275A4
EP2968275A4 EP14763091.7A EP14763091A EP2968275A4 EP 2968275 A4 EP2968275 A4 EP 2968275A4 EP 14763091 A EP14763091 A EP 14763091A EP 2968275 A4 EP2968275 A4 EP 2968275A4
Authority
EP
European Patent Office
Prior art keywords
lxr modulators
lxr
modulators
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP14763091.7A
Other languages
German (de)
English (en)
Other versions
EP2968275B1 (fr
EP2968275A1 (fr
Inventor
Ellen K Kick
Mandar Bodas
Raju Mohan
Meriah Valente
Nicholas Wurtz
Sharanabasappa Patil
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Exelixis Patent Co LLC
Original Assignee
Bristol Myers Squibb Co
Exelixis Patent Co LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co, Exelixis Patent Co LLC filed Critical Bristol Myers Squibb Co
Publication of EP2968275A1 publication Critical patent/EP2968275A1/fr
Publication of EP2968275A4 publication Critical patent/EP2968275A4/fr
Application granted granted Critical
Publication of EP2968275B1 publication Critical patent/EP2968275B1/fr
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
EP14763091.7A 2013-03-15 2014-03-14 Modulateurs des lxr Active EP2968275B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361786974P 2013-03-15 2013-03-15
PCT/US2014/028274 WO2014144037A1 (fr) 2013-03-15 2014-03-14 Modulateurs des lxr

Publications (3)

Publication Number Publication Date
EP2968275A1 EP2968275A1 (fr) 2016-01-20
EP2968275A4 true EP2968275A4 (fr) 2016-08-10
EP2968275B1 EP2968275B1 (fr) 2017-11-29

Family

ID=51537598

Family Applications (1)

Application Number Title Priority Date Filing Date
EP14763091.7A Active EP2968275B1 (fr) 2013-03-15 2014-03-14 Modulateurs des lxr

Country Status (5)

Country Link
US (1) US9834542B2 (fr)
EP (1) EP2968275B1 (fr)
JP (1) JP6442475B2 (fr)
CN (1) CN105209039B (fr)
WO (1) WO2014144037A1 (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6456909B2 (ja) 2013-03-15 2019-01-23 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｌｘｒ調節因子
US10669296B2 (en) 2014-01-10 2020-06-02 Rgenix, Inc. LXR agonists and uses thereof
CN104817525B (zh) * 2015-04-13 2017-11-17 江苏大学 含氟2,3‑二氢苯并呋喃‑3‑醇类化合物及制备方法
CA3010883A1 (fr) 2016-01-11 2017-07-20 The Rockefeller University Methodes pour le traitement de troubles associes a des cellules suppressives derivees de cellules myeloides
CA3078981A1 (fr) 2017-11-21 2019-05-31 Rgenix, Inc. Polymorphes et leurs utilisations
CN109867645B (zh) * 2017-12-05 2021-09-14 中国医学科学院药物研究所 一种2,2-二氟-2,3-二氢取代苯并呋喃类化合物的合成方法
TWI748194B (zh) * 2018-06-28 2021-12-01 德商菲尼克斯 Ｆｘｒ有限責任公司 含有雙環核心部分之新穎lxr調節劑
CN110330493B (zh) * 2019-08-23 2020-07-24 广州麓鹏制药有限公司 Pim激酶抑制剂、其制备方法、应用、药物及药物组合
AU2020401286A1 (en) 2019-12-13 2022-06-23 Inspirna, Inc. Metal salts and uses thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120071534A1 (en) * 2009-05-28 2012-03-22 Busch Brett B Lxr modulators
WO2012135082A1 (fr) * 2011-03-25 2012-10-04 Bristol-Myers Squibb Company Promédicaments de dérivés d'imidazole modulant lxr

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US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4444784A (en) 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
MX7065E (es) 1980-06-06 1987-04-10 Sankyo Co Un procedimiento microbiologico para preparar derivados de ml-236b
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
HU204253B (en) 1982-11-22 1991-12-30 Sandoz Ag Process for producing mevalonolactone analogues and derivatives and pharmaceutical compositions containing them
DE3779500T2 (de) 1986-06-10 1993-01-21 Chiesi Farma Spa Levodopa-methyl-ester enthaltende pharmazeutische zusammensetzungen, ihre herstellung und therapeutische verwendungen.
US5138069A (en) 1986-07-11 1992-08-11 E. I. Du Pont De Nemours And Company Angiotensin II receptor blocking imidazoles
US5506219A (en) 1988-08-29 1996-04-09 E. R. Squibb & Sons, Inc. Pyridine anchors for HMG-CoA reductase inhibitors
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
US5177080A (en) 1990-12-14 1993-01-05 Bayer Aktiengesellschaft Substituted pyridyl-dihydroxy-heptenoic acid and its salts
US5854265A (en) 1996-04-03 1998-12-29 Merck & Co., Inc. Biheteroaryl inhibitors of farnesyl-protein transferase
WO1997036881A1 (fr) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibiteurs de la farnesyl-proteine transferase
EP0891356A1 (fr) 1996-04-03 1999-01-20 Merck & Co., Inc. Inhibiteurs de la farnesyl-proteine transferase
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WO1998032444A1 (fr) 1997-01-24 1998-07-30 The Regents Of The University Of California UTILISATION D'ACTIVATEURS DE FXR, PPARα ET LXRα DANS LE BUT DE RESTAURER LA FONCTION DE BARRIERE, DE FAVORISER LA DIFFERENCIATION EPIDERMIQUE ET D'INHIBER LA PROLIFERATION EPIDERMIQUE
EP1059843A1 (fr) 1998-02-25 2000-12-20 Merck & Co., Inc. Procede de reduction de l'allongement de l'espace qt ou d'inhibition de l'allongement de l'espace qt a l'aide d'un antagoniste de recepteur de l'angiotensine ii
EP1115853A2 (fr) 1998-09-23 2001-07-18 Ludmila Solomin Analyse de recepteurs nucleaires actives par des ligands in vivo
US6639078B1 (en) 1998-12-23 2003-10-28 Smithkline Beecham Corporation Assays for ligands for nuclear receptors
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WO2001082917A2 (fr) 2000-05-03 2001-11-08 Tularik Inc. Traitement de l'hypertriglyceridemie et d'autres maladies au moyen de modulateurs lxr
AU2001273040A1 (en) 2000-06-27 2002-01-08 Du Pont Pharmaceuticals Company Factor xa inhibitors
US6924311B2 (en) 2001-10-17 2005-08-02 X-Ceptor Therapeutics, Inc. Methods for affecting various diseases utilizing LXR compounds
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WO2003059884A1 (fr) 2001-12-21 2003-07-24 X-Ceptor Therapeutics, Inc. Modulateurs de lxr
AU2006261841B8 (en) 2005-06-27 2012-12-06 Exelixis Patent Company Llc Pyrazole based LXR modulators
US7741317B2 (en) 2005-10-21 2010-06-22 Bristol-Myers Squibb Company LXR modulators
KR20090094125A (ko) 2006-12-08 2009-09-03 엑셀리시스, 인코포레이티드 Ｌｘｒ 및 ｆｘｒ 조절자
JP6456909B2 (ja) 2013-03-15 2019-01-23 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｌｘｒ調節因子

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120071534A1 (en) * 2009-05-28 2012-03-22 Busch Brett B Lxr modulators
WO2012135082A1 (fr) * 2011-03-25 2012-10-04 Bristol-Myers Squibb Company Promédicaments de dérivés d'imidazole modulant lxr

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of WO2014144037A1 *

Also Published As

Publication number Publication date
JP6442475B2 (ja) 2018-12-19
EP2968275B1 (fr) 2017-11-29
CN105209039A (zh) 2015-12-30
CN105209039B (zh) 2018-06-22
US20160304499A1 (en) 2016-10-20
US9834542B2 (en) 2017-12-05
WO2014144037A1 (fr) 2014-09-18
EP2968275A1 (fr) 2016-01-20
JP2016513730A (ja) 2016-05-16

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